Multifunctional theranostic nanodevices carrying therapeutic payloads, diagnostic agents, and targeted and controlled drug release functions can simultaneously and effectively diagnose and treat cancers. The targeted delivery of chemotherapeutics to tumors can significantly increase the efficacy of drugs while minimizing the severe side effects associated with the drug itself. The integration of the four functions into one single platform holds great promise for increasing therapeutic index and improving patient outcome. The proposed theranostic nanodevice by Luna Innovations will be tested in both cell culture experiments and in vivo small animal studies during the Phase I period. Each component of the integrated nanodevice has been designed to carry its specific function of loading anticancer drugs, preventing the drug from premature release, triggering drug release when it reaches its intended region of action, guiding the nanodevice to tumor sites, inhibiting the growth of cancerous cells, or monitoring the tumor regression by MR imaging. Luna anticipates that both of the in vitro and in vivo results will validate the design of the multifunctional nanodevice and demonstrate the feasibility of the nanodevice for simultaneous diagnosis and treatment of tumors. These results will provide a foundation for full R&D efforts in Phase II.